摘要:
The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that the 3a and 6a hydrogens are cis and where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens, andwith the proviso that R.sup.b is not hydrogen when the 4-position aryl is cis to the 3a and 6a hydrogens and there is no hydroxy at the 4-position.
摘要:
Octahydroindolizidines and corresponding ketones of the formulae (I) and (II): ##STR1## where A is a 3-7 carbon or hetero-containing ring, R.sup.1 is a substituent, n is 0-6 and x is 0-3. Also, pharmaceutical compositions for treating pain containing (I) or (II) and methods for synthesis and use as well as novel intermediates in the synthesis. A
摘要:
The 4-arylcyclopenta[c]pyrroles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that where there is a 4-position hydroxy then such is trans to the 3a and 6a hydrogens.
摘要:
The 4-arylisoindoles of the following formula are effective analgesics: ##STR1## including stereoisomers and pharmaceutically acceptable salts thereof, wherein ##STR2## with the proviso that there is 0 or 1 unsaturated bond in the isoindole ring and with the proviso that where the stereoisomer is:a) the 3a.beta., 4.beta., 7a.alpha. diastereomer, then a double bond joins the 5- and 6-position carbons or the 6- and 7-position carbons;b) the 3a.beta., 4.alpha., 7a.alpha. or the 3a.beta., 4.alpha., 7a.beta. diastereomers, then the double bond joins the 5- and 6-position carbons; andc) the 3a.beta., 4.beta., 7a.beta. diastereomer, then the double bond joins the 6- and 7-position carbons.
摘要:
Loweralkyl 1-methylpyrrole-2-acetates are prepared by the recuction of loweralkyl .alpha.-imino-1-methylpyrrole-2-acetates using a divalent sulfur reducing agent.
摘要:
Aroyl(piperidinyl and piperazinyl)acyl pyrroles of the following formula have anxiolytic activity: ##STR1## wherein, Y is selected from the group consisting of N, CH or COH;A.sup.1 is selected from the group consisting of ##STR2## n is an integer from 1 to 5; R1 is selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.2 and R.sup.3 are selected from the group consisting of H and C.sub.1-4 alkyl;R.sup.4 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; andR.sup.5 is selected from the group consisting of halo, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy, nitro, amino, C.sub.1-4 acylamino, cyano, trihaloC.sub.1-4 alkyl, C.sub.1-4 alkylsulfonyl, C.sub.1-4 alkylsulfinyl and C.sub.1-4 acyl; and acid addition salts thereof.
摘要翻译:下式的芳酰基(哌啶基和哌嗪基)酰基吡咯具有抗焦虑活性:p由N,CH或COH组成; A1选自 + TR ,n是1至5的整数; R 1选自H和C 1-4烷基; R2和R3选自H和C1-4烷基; R 4选自卤素,C 1-4烷基,羟基,C 1-4烷氧基,硝基,氨基,C 1-4酰氨基,氰基,三卤代C 1-4烷基,C 1-4烷基磺酰基,C 1-4烷基亚磺酰基和C 1-4酰基; R 5选自卤素,C 1-4烷基,羟基,C 1-4烷氧基,硝基,氨基,C 1-4酰氨基,氰基,三卤代C 1-4烷基,C 1-4烷基磺酰基,C 1-4烷基亚磺酰基和C 1-4酰基; 及其酸加成盐。
摘要:
Hexahydropyrrolizines of the formula (I): ##STR1## wherein A is a 3-7 carbon or hetero-containing ring,R.sup.1 is a substituent, andx is 0-3.Also, pharmaceutical compositions for treating pain and methods for synthesis and use as well as novel intermediates in the synthesis.
摘要:
Octahydroquinolizine and corresponding octahydroquinolizinium compounds of formulae (I) and (Va): ##STR1## where A is a 3 to 7 membered carbocyclic ring, R.sup.1 is a substituent, n is 0-2, x is 0-3, and Y is an anion. Also, pharmaceutical compositions for treating pain containing (I) and methods for synthesis and use as well as novel intermediates in the synthesis.
摘要:
4-[aryl(piperidin-4-yl)]aminobenzamides are delta-opioid receptor agonists/antagonists. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their agonist/antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of mental illness, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents, and agents for the treatment of respiratory diseases.
摘要:
The 4-arylisoindoles of the following formula are effective analgesics: ##STR1## including the purified stereoisomers and pharmaceutically acceptable salts thereof,wherein ##STR2## R.sup.b is hydroxy or C.sub.1-5 alkylcarbonyloxy.